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image of Formulation and Characterization of Multiparticulate System for Proton Pump Inhibitor using Combination Therapy for Peptic Ulcer

Abstract

Introduction

The purpose of this study was to develop sustained-release enteric-coated granules of Amla extract and esomeprazole magnesium for the treatment of peptic ulcer. It is well known that Amla possesses anti-ulcer activity due to the phenolic compound gallic acid, which inhibits a gastric H+/K+ ATPase pump. Therefore, enteric-coated Amla extract granules were combined with esomeprazole magnesium granules to enhance the synergistic effect, mitigate adverse effects associated with esomeprazole magnesium, and improve overall anti-ulcer activity, while the enteric-coated multiparticulate system ensures prolonged drug release with a minimum dose.

Methods

A Soxhlet extraction method was employed to obtain the Amla phenolic extract, using a solvent mixture of ethanol and water in a 7:3 ratio. Wet granulation techniques were utilized to prepare granules, and hydroxypropyl methylcellulose phthalate served as the enteric coating agent. The drug release and drug entrapment were used to optimize the enteric-coated granules of Amla extract and Esomeprazole Magnesium. An study was conducted in Wistar albino rats (120-140 g) of both sexes to demonstrate the antiulcer activity of the developed formulation against an aspirin-induced ulcerated rat model.

Results

Both and studies were conducted. In the studies, drug release was assessed at pH 1.2 (simulated gastric fluid) and pH 6.8 (simulated intestinal fluid). The results demonstrated negligible drug release in the simulated gastric fluid due to the protective enteric coating, while efficient drug release occurred in the simulated intestinal fluid. In the studies, the combination therapy showed a significant therapeutic effect compared to other treatment groups in an animal model.

Discussion

Amla extract and esomeprazole magnesium were combined to prepare sustained-release enteric-coated granules for the treatment of peptic ulcers. The phenolic substance gallic acid inhibits the gastric H+/K+ ATPase pump, thereby enhancing anti-ulcer efficacy. The combination demonstrated substantial therapeutic efficacy in both and investigations.

Conclusion

The amla extract and esomeprazole magnesium enteric-coated granules with sustained release and negligible drug release in acidic pH were achieved. In the studies, the combination therapy demonstrated a significant positive effect in treating peptic ulcers in a rat ulcer model, as shown by assessments of various parameters such as ulcer index, total gastric juice acidity, hematological analysis, and histopathological evaluations.

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2025-07-14
2025-09-10

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Formulation and Characterization of Multiparticulate System for Proton Pump Inhibitor using Combination Therapy for Peptic Ulcer
Bentham Science Publishers ; https://doi.org/10.2174/0126673878360081250628164032
/content/journals/raddf/10.2174/0126673878360081250628164032
/content/journals/raddf/10.2174/0126673878360081250628164032
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  • Article Type:     Research Article
Keywords: amla extract ; esomeprazole magnesium ; drug release ; in vivo study ; Peptic ulcer ; drug entrapment

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